Antibacterial steroidal alkaloids from Holarrhena antidysenteriaca / 中国天然药物

Two new steroidal alkaloids, isoconkuressine and N-formylconessimine, together with 6 known steroidal alkaloids including conkuressine, conessine, isoconessimine, conimine, conarrhimine, and funtudienine, were isolated from the seeds of Holarrhena antidysenteriaca Wall.ex A.DC. Their intrinsic antibacterial activities and synergistic effects with penicillin and vancomycin were analyzed in methicillin sensitive staphylococcus aureus (MSSA) and methicillin resistant staphylococcus aureus (MRSA). Two of the steroidal alkaloids including one new compound (N-formylconessimine) showed potential antibacterial activity and possessed synergistic effects with penicillin and vancomycin, respectively.

In vitro cytotoxic activity of leaves extracts of Holarrhena antidysenterica against some human cancer cell lines.

In vitro cytotoxic potential of extracts (95% and 50% ethanolic extract and hot water extract at concentration of 100 µg/ml) from leaves of Holarrhena antidysenterica was evaluated against fourteen human cancer cell lines — A-549, COLO-205, DU-145, HeLa, HEP-2, IMR-32, KB, MCF-7, NCI-H23, OVCAR-5, SiHa, SK-N-MC, SW-620 and ZR-75-1 from nine different tissues (breast, colon, cervix, CNS, lung, liver, oral, ovary and prostate) using SRB assay. The 95% ethanolic extract displayed maximum anti-proliferative effect in the range of 73-92% against eight human cancer cell lines, while 50% ethanolic extract showed cytotoxic activity in the range of 70-94% against seven human cancer cell lines. However, the hot water extract did not show any activity. Among the fractions of 95% and 50% ethanolic extract, significant cytotoxic activity was found in the chloroform soluble fraction of 95% ethanolic extract at 100 µg/ml; it inhibited the growth in the range of 71-99% of seven human cancer cell lines from five different tissues viz., OVCAR-5 (ovary), HT-29 (colon), SK-N-MC (neuroblastoma), HEP-2 (liver), COLO-205 (colon), NIH-OVCAR-3 (ovary) and A-549 (lung). The cytotoxic activity of chloroform soluble fraction was found to be higher than 5-flurouracil, adriamycin, mitomycin-c and paclitaxel (anticancer drugs used as positive controls). Further in vivo studies and identification of active components from the chloroform fraction and their exact mechanism of action could be useful in designing new anticancer therapeutic agents.

Pharmacodynamic evaluation for antiplasmodial activity of Holarrhena antidysentrica (Kutaja) and Azadirachta indica (Neemb) in Plasmodium berghei infected mice model

OBJECTIVE@#To investigate in-vivo anti-plasmodial activity of aqueous extracts of plants selected based on the symptomology mentioned in Ayurveda.@*METHODS@#The aqueous extracts of Holarrhena antidysentrica (H. antidysentrica) (Kutaja) and Azadirachta indica (A. indica) (Neemb) for their antiplasmodial potential in Plasmodium berghei (P. berghei) infected mice was assessed using Peters four day suppressive test. Both the extracts were administered at 2 dose levels, full dose (1 000 mg/d) and minimized dose (200 mg/d). 10(6)P. berghei infected RBCs were injected on day '0' and treated from day '0' till day '3' post-infection. Tail blood smears were collected, giemsa stained and analyzed. The mice were observed for survival and parasitemia was assessed till 50% of mice in control survived.@*RESULTS@#It was observed that the percentage of parasitemia increased gradually in all the groups, with maximum in control group (Day 3-35, Day 9-46.98) and minimum in Chloroquine arm (Day 3-14.06, Day 9-19.92). The percentage of parasitemia was compared using Mann-Whitney U test depicting that all test groups exhibited reduction in parasitemia as compared to control (P-value<0.002 for all groups). These groups showed similar percentage of survival as Chloroquine.@*CONCLUSIONS@#The present investigation demonstrated the anti-plasmodial effects of H. antidysentrica and A. indica, which are two most commonly used medicinal plants in Ayurved for treatment of fever.

Studying of flavonoids in the leaves of Holarrhena antidysenterica Wall

The study on Holarrhena antidysenterica Wall was carried out in Chi Linh (Hai Duong province) in September 2004. Leaves of Holarrhena antidysenterica Wall were collected, dried, grilled to powder, then extracted and isolated flavonoid. Two flavonoids were isolated, on the base of m.p, UV, IR, MS, 1H-NMR, 13C-NMR, DEPT analyses, they were identified as Kaempferol and Quercetin. This is the first time the flavonoids were reported as a substance isolated from Holarrhena antidysenterica Wall in Vietnam

Antibacterial and antidiarrhoeal effects of alkaloids of Holarrhena antidysenterica WALL.

The alkaloids from the ethanolic extract of H. antidysenterica seeds were evaluated for their antibacterial activity against clinical isolates of enteropathogenic Escherichia coli (EPEC) in vitro, and their antidiarrhoeal activity on castor oil-induced diarrhoea in rats, in vivo. The plasmid DNA, whole cell lysate and outer membrane protein profile of a clinical isolate of EPEC was determined in presence of alkaloids of H. antidysenterica. The disc diffusion and agar well diffusion methods were used to evaluate the antibacterial efficacy. The alkaloids showed strong antibacterial activity against EPEC strains. In castor oil-induced diarrhoea, alkaloids reduced the diarrhoea with decrease in the number of wet faeces in pretreated rats at a dose of 200-800 mg/kg. The loss of plasmid DNA and suppression of high molecular weight proteins were observed on alkaloids treatment. Taking into account the multiple antibiotic resistance of EPEC, the results suggest usefulness of alkaloids of H. antidysenterica seeds as antibacterial and antidiarrhoeal agents.